3rkz

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[[Image:3rkz.png|left|200px]]
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==Discovery of a stable macrocyclic o-aminobenzamide Hsp90 inhibitor capable of significantly decreasing tumor volume in a mouse xenograft model.==
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<StructureSection load='3rkz' size='340' side='right' caption='[[3rkz]], [[Resolution|resolution]] 1.57&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[3rkz]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3RKZ OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3RKZ FirstGlance]. <br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=06T:(5R,6S)-3-(L-ALANYL)-5,6,15,15,18-PENTAMETHYL-17-OXO-2,3,4,5,6,7,14,15,16,17-DECAHYDRO-1H-12,8-(METHENO)[1,5,9]TRIAZACYCLOTETRADECINO[1,2-A]INDOLE-9-CARBOXAMIDE'>06T</scene></td></tr>
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<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">HSP90A, HSP90AA1, HSPC1, HSPCA ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])</td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3rkz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3rkz OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3rkz RCSB], [http://www.ebi.ac.uk/pdbsum/3rkz PDBsum]</span></td></tr>
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</table>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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An extension of our previously reported series of macrocyclic ortho-aminobenzamide Hsp90 inhibitors is reported. Addition of a second methyl group to the tether provided analogs that show increased potency in binding as well as cell-proliferation assays and, more importantly, are stable toward microsomes. We wish to disclose the discovery of a macrocycle which showed impressive biomarker activity 24-h post dosing and which demonstrated prolonged exposure in tumors. When studied in a lung cancer xenograft model, the compound demonstrated significant tumor size reduction.
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{{STRUCTURE_3rkz| PDB=3rkz | SCENE= }}
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Discovery of a stable macrocyclic o-aminobenzamide Hsp90 inhibitor which significantly decreases tumor volume in a mouse xenograft model.,Zapf CW, Bloom JD, Li Z, Dushin RG, Nittoli T, Otteng M, Nikitenko A, Golas JM, Liu H, Lucas J, Boschelli F, Vogan E, Olland A, Johnson M, Levin JI Bioorg Med Chem Lett. 2011 Jun 27. PMID:21715165<ref>PMID:21715165</ref>
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===Discovery of a stable macrocyclic o-aminobenzamide Hsp90 inhibitor capable of significantly decreasing tumor volume in a mouse xenograft model.===
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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{{ABSTRACT_PUBMED_21715165}}
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==About this Structure==
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[[3rkz]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3RKZ OCA].
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==See Also==
==See Also==
*[[Heat Shock Proteins|Heat Shock Proteins]]
*[[Heat Shock Proteins|Heat Shock Proteins]]
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== References ==
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==Reference==
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<references/>
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<ref group="xtra">PMID:021715165</ref><references group="xtra"/>
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__TOC__
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</StructureSection>
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Bloom, J D.]]
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[[Category: Bloom, J D]]
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[[Category: Boschelli, F.]]
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[[Category: Boschelli, F]]
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[[Category: Dushin, R G.]]
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[[Category: Dushin, R G]]
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[[Category: Golas, J M.]]
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[[Category: Golas, J M]]
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[[Category: Johnson, M.]]
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[[Category: Johnson, M]]
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[[Category: Levin, J I.]]
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[[Category: Levin, J I]]
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[[Category: Li, Z.]]
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[[Category: Li, Z]]
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[[Category: Liu, H.]]
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[[Category: Liu, H]]
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[[Category: Lucas, J.]]
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[[Category: Lucas, J]]
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[[Category: Nikitenko, A.]]
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[[Category: Nikitenko, A]]
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[[Category: Nittoli, T.]]
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[[Category: Nittoli, T]]
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[[Category: Olland, A.]]
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[[Category: Olland, A]]
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[[Category: Otteng, M.]]
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[[Category: Otteng, M]]
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[[Category: Vogan, E.]]
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[[Category: Vogan, E]]
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[[Category: Zapf, C W.]]
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[[Category: Zapf, C W]]
[[Category: Atp binding domain]]
[[Category: Atp binding domain]]
[[Category: Atp-binding]]
[[Category: Atp-binding]]

Revision as of 12:34, 9 December 2014

Discovery of a stable macrocyclic o-aminobenzamide Hsp90 inhibitor capable of significantly decreasing tumor volume in a mouse xenograft model.

3rkz, resolution 1.57Å

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